Synthesis and structure–activity relationships of 2-aryl-4-oxazolylmethoxy benzylglycines and 2-aryl-4-thiazolylmethoxy benzylglycines as novel, potent PPARα …

…, KT Locke, K O'Malley, L Zhang, R Srivastava…

文献索引：Ye, Xiang-Yang; Chen, Stephanie; Zhang, Hao; Locke, Kenneth T.; O'Malley, Kevin; Zhang, Litao; Srivastava, Raijit; Miao, Bowman; Meyers, Daniel; Monshizadegan, Hossain; Search, Debra; Grimm, Denise; Zhang, Rongan; Lippy, Jonathan; Twamley, Celeste; Muckelbauer, Jodi K.; Chang, Chiehying; An, Yongmi; Hosagrahara, Vinayak; Zhang, Lisa; Yang; Mukherjee, Ranjan; Cheng, Peter T.W.; Tino, Joseph A. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 9 p. 2933 - 2937

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被引用次数: 6

摘要

The synthesis and follow-up SAR studies of our development candidate 1 by incorporating 2- aryl-4-oxazolylmethoxy and 2-aryl-4-thiazolylmethoxy moieties into the oxybenzylglycine framework of the PPARα/γ dual agonist muraglitazar is described. SAR studies indicate that different substituents on the aryloxazole/thiazole moieties as well as the choice of carbamate substituent on the glycine moiety can significantly modulate the selectivity of PPARα ...